The synthesis of BOL-148 in the United States and many other countries is plagued with a handful of regulatory and chemistry issues. The first synthesis of 2-Bromo-LSD (BOL-148) comprised reacting 13.2 grams of N-bromosuccinimide (in 400 mL dioxane) with 1.2 liters of dioxane containing 25 grams of LSD. This gave 11 grams of crude product, which had to be recrystallized. The radioactive synthesis uses effectively elemental bromine, and provided yields ranging from 5 to 15%.
LSD is a schedule one drug in the United States and beginning in 1968 the United Nations Economic and Social Council (ECOSOC) passed a resolution calling on nations to limit the use of such drugs to scientific and medical purposes and to impose import and export restrictions. In accordance with the Convention on Psychotropic Substances of 1971, the International Narcotics Control Board listed LSD as Schedule 1 for United Nations member countries. Additionally, in 1988 the United Nations listed Ergometrine, Ergotamine, and Lysergic Acid under table 1 as precursors. Furthermore, the United States DEA covers Egonovine and Ergocristine as List 1 precursors.
The above regulations contribute to the overhead costs, regulatory resources, and additional expenses and permitting depending on the route chosen to manufacture BOL-148.
It would be beneficial to develop a synthetic method which overcomes these and other issues. Indeed, it would be beneficial to develop a method which eliminates any registration, importation permits, and/or controlled substance handling permits. It would also be beneficial to be able to develop a synthetic strategy that utilizes starting materials that are cost effective, readily available, and unregulated in use.